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Pimitespib

Catalog No. T16994 CAS 1260533-36-5

Synonyms: TAS-116

Pimitespib (TAS-116) is an ATP-competitive and highly specific HSP90α/HSP90β inhibitor (Kis: 34.7 nM and 21.3 nM, respectively).

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Pimitespib, CAS 1260533-36-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 378.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 99.49%

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Description	Pimitespib (TAS-116) is an ATP-competitive and highly specific HSP90α/HSP90β inhibitor (Kis: 34.7 nM and 21.3 nM, respectively).
Targets&IC50	HSP90 β:21.3 nM (Ki), HSP90 α:34.7 nM (Ki)
In vitro	TAS-116 binds not only to the conventional-binding pockets as existing Hsp-90 inhibitors but also to a novel-binding pocket. Such a unique binding mode makes TAS-116 highly specific for Hsp-90α/β. TAS-116 (0-5 μM, 48 hours) inhibits human retinal pigment epithelial ARPE-19 cell lines and NCI-H929 MM cell growth. Compared 17-AAG in INA6 and NCI-H929 MM cells, more significant degradation of p-C-Raf and p-MEK1/2, HSP90 client proteins, and key RAS/RAF/MEK pathway regulators, is triggered by TAS-116 (0.125-1 μM, 24 hours) [2][3].
In vivo	TAS-116 is orally absorbed and has a bioavailability of almost 100% in mice, and 69.0% in rats. TAS-116 has moderate terminal elimination half-life (t1/2=8.2 h, 2.5 h, 4.4 h and 2.2 h for mouse (3.6 mg/kg, p.o.), mouse (7.1 mg/kg, p.o.), mouse (14.0 mg/kg, p.o.), rat (4 mg/kg, p.o.)). TAS-116 is more rapidly eliminated from retina (t1/2=3.4 hours) than the other HSP90 inhibitors (t1/2=7.1-19.1 hours). TAS-116 is distributed less in retina than in plasma in rats; consequently, TAS-116 does not produce any detectable photoreceptor injury. TAS-116 triggers enhanced in vivo anti-MM activities, both alone and in combination with Bortezomib (BTZ), with a favorable safety profile. TAS-116 (12.0 mg/kg, p.o., 14 days) displays antitumor activity without inducing eye injury in rats. Mice treated with TAS-116 (10 mg/kg and 15 mg/kg, orally, 38 days), BTZ, or TAS-116 plus BTZ show significantly enhance growth inhibition versus the vehicle control group. Median overall survival of treated animals (TAS-116, orally, 10 mg/kg=33 days, 15 mg/kg=37 days, BTZ=36 days, and the combination=56.5 days) is significantly longer than vehicle control. The favorable pharmacokinetic profile of TAS-116 is reflected in its dose-dependent antitumor activity; the T/C (tumor volume of TAS-116-treated mice vs. vehicle-treated mice) is 47%, 21%, and 9% for doses of 3.6 mg/kg, 7.1 mg/kg, and 14.0 mg/kg, respectively [1][2].

Synonyms	TAS-116
Molecular Weight	454.53
Formula	C25H26N8O
CAS No.	1260533-36-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (275.01 mM), Sonication is recommended.

References and Literature

1. Ohkubo S, et al. TAS-116, a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models. Mol Cancer Ther. 2015 Jan;14(1):14-22. 2. Suzuki R, et al. Anti-tumor activities of selective HSP90α/β inhibitor, TAS-116, in combination with bortezomib in multiple myeloma. Leukemia. 2015 Feb;29(2):510-4. 3. Utsugi T. New challenges and inspired answers for anticancer drug discovery and development. Jpn J Clin Oncol. 2013 Oct;43(10):945-53.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library NO PAINS Compound Library Clinical Compound Library Endoplasmic Reticulum Stress Compound Library Cytoskeletal Signaling Pathway Compound Library Exosome Compound Library

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Keywords

Pimitespib 1260533-36-5 Cytoskeletal Signaling Metabolism HSP inhibit TAS116 TAS-116 TAS 116 Heat shock proteins Inhibitor inhibitor

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